State Key Laboratory of Chemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, PR China.
Beijing Institute for Brain Disorders, Capital Medical University, Beijing 100069, China.
Int J Biol Macromol. 2022 Jul 31;213:1057-1067. doi: 10.1016/j.ijbiomac.2022.06.046. Epub 2022 Jun 9.
This study aimed to prepare alcohol-free curcumin-loaded zein-propylene glycol alginate (zein-PGA-Cur) nanoparticles using the pH-driven method to enhance the bioavailability and physicochemical stability of curcumin. The prepared zein-PGA-Cur nanoparticles exhibited a small size (360 nm) and negative zeta-potential (-5.8 mV), as well as excellent physical stability, under storage conditions of pH 4.0 and temperature at 4 °C for 30 days. In addition, the Fourier transform infrared spectroscopy results demonstrated that the main interactions of pH-driven for the formation of zein-PGA-Cur nanoparticles were hydrogen bonding, hydrophobic, and electrostatic interactions. Fluorescence spectroscopy revealed that the curcumin-induced fluorescence quenching of zein was static. Circular Dichroism spectroscopy demonstrated that the pH-driven method mainly decreased the β-sheet structure of zein from 3.9 % to 1.4 %. Furthermore, the HT-29 colorectal adenocarcinoma cells viability experiments revealed that the prepared zein-PGA-Cur nanoparticles exhibited excellent biocompatibility. In vivo rat experiments also demonstrated that the prepared nanoparticles resulted in a higher plasma concentration of curcumin, representing a 7.2-fold enhancement in bioavailability compared with pure curcumin crystals. The findings of this study will provide a green and energy-saving method for the development of insoluble drug self-assembly systems and promote their wider applications in drug delivery.
本研究旨在使用 pH 驱动法制备无醇姜黄素负载的玉米醇溶蛋白-丙二醇藻酸盐（zein-PGA-Cur）纳米粒，以提高姜黄素的生物利用度和物理化学稳定性。在 pH 4.0 和 4°C 的储存条件下，制备的 zein-PGA-Cur 纳米粒具有小尺寸（360nm）和负 zeta 电位（-5.8mV），以及出色的物理稳定性，在 30 天内。此外，傅里叶变换红外光谱结果表明，pH 驱动形成 zein-PGA-Cur 纳米粒的主要相互作用是氢键、疏水和静电相互作用。荧光光谱表明，姜黄素诱导的玉米醇溶蛋白荧光猝灭是静态的。圆二色性光谱表明，pH 驱动法主要使玉米醇溶蛋白的β-折叠结构从 3.9%降低至 1.4%。此外，HT-29 结肠直肠腺癌细胞活力实验表明，所制备的 zein-PGA-Cur 纳米粒具有优异的生物相容性。体内大鼠实验还表明，所制备的纳米粒使姜黄素的血浆浓度更高，生物利用度提高了 7.2 倍，与纯姜黄素晶体相比。本研究的结果将为开发不溶性药物自组装系统提供一种绿色节能的方法，并促进其在药物输送中的更广泛应用。
